对氨基苯甲酸置于copper(I) Bromide Potassium Nitrite,氢溴酸,二甲基亚砜体系中,用 水 作为反应溶剂,化学反应 0.17H,以83%的收率获得产物4-溴苯甲酸 参考文献:Efficient One-Pot Transformation Of Aminoarenes To Haloarenes Using Halodimethylisulfonium Halides Generated In Situ 标题:Efficient One-Pot Transformation Of Aminoarenes To Haloarenes Using Halodimethylisulfonium Halides Generated In Situ 摘要:卤二甲基亚砜卤化物1是一种非常好的亲核卤化物,可在现场由氢卤酸和二甲亚砜形成.这种活化的亲核卤化物迅速将由相同的氢卤酸和亚硝酸根在现场制备的芳基重氮盐转化为芳基氯化物,溴化物或碘化物,收率较高.在dmso中,亚硝酸根和氢卤酸的联合作用是直接转化芳香胺的必要条件,从而在1小时内产生芳基卤化物.带有电子给体或吸引基团或有立体位阻的芳香胺的取代化合物也可顺利转化为相应的芳香卤化物.观测到的唯一副产物是去氨基芳烃(通常<7%).孤立的芳基重氮盐也可以使用1转化为相应的芳基卤化物.该方法提供了一种简便的,一步法的程序,用于将氨基芳烃转化为卤代芳烃,并且不伴随通常伴随使用铜卤化物进行桑迈尔反应的环境污染物.关键词:氨基芳烃,卤代芳烃,卤二甲基亚砜卤化物,卤化,胺化. DOI:10.1139/v05-026
专利号:US-11999757-B2 优先权日:2017-11-01 标 题:Synthesis of boronate ester derivatives and uses thereof 发明人:BOYER SERGE HENRI; HECKER SCOTT J; VERZIJL GERARDUS K M; HERMSEN PETRUS J 权利人:MELINTA SUBSIDIARY CORP 摘要:Disclosed herein are methods for the preparation of boronate derivatives in the synthesis of antimicrobial compounds and uses thereof. Disclosed herein includes method of making a compound of Formula (B) by reducing the ketone group of the keto-ester compound of Formula (A), and the reduction can be performed using a Ruthenium based catalyst system or using an alcohol dehydrogenase bioreduction system.
专利号:US-10669292-B2 优先权日:2014-05-05 标 题 :Synthesis of boronate salts and uses thereof 发明人:HECKER SCOTT; BOYER SERGE 权利人:REMPEX PHARMACEUTICALS INC 摘要:Disclosed herein are boronate intermediates in the synthesis of antimicrobial compounds and the use and preparation thereof. Some embodiments relate to crystalline boronate salt derivatives and their use in the synthesis of therapeutic compounds.
专利号:US-7816544-B2 优先权日:2004-03-23 标 题:Synthesis of rocaglamide natural products via photochemical generation of oxidopyrylium species 发明人:JONES II GUILFORD; GERARD BAUDOUIN; PORCO JR JOHN A 权利人:UNIV BOSTON 摘要:The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.
专利号:US-11407993-B2 优先权日:2017-02-14 标 题 :Method for the synthesis of DNA conjugates by micellar catalysis 发明人:BHAT AVINASH SHASHIDHAR; KLIKA SKOPIC MATEJA; BRUNSCHWEIGER ANDREAS; WEBERSKIRCH RALF 权利人:UNIV DORTMUND TECH 摘要:A method for the synthesis of a chimeric conjugate molecule by micellar catalysis that may form part of DNA-encoded compound libraries. A DNA-coupled organic starter molecule may be reacted with another organic compound, using a catalyst located within a micelle, to form a conjugate of an organic candidate compound coupled to a DNA identifier tag.
专利号:US-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
专利号:EP-1641729-B1 优先权日:2003-07-09 标题:Use of functionalized onium salts as a soluble support for organic synthesis 发明人:VAULTIER MICHEL; GMOUH SAID; HASSINE FATIMA 权利人:CENTRE NAT RECH SCIENT; UNIV RENNES 摘要:The invention relates to the use of a onium salt functionalized by at least one organic function, as a soluble support, in the presence of at least one organic solvent, for organic synthesis of a molecule, in a homogenous phase, by at least one transformation of said organic function. The onium salt enables the synthesized molecule to be released. The onium salt is present in liquid or solid form at room temperature and corresponds to formula A1+, X1-, wherein A1+ represents a cation and X1- represents an anion.
摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 555. 摘要:Wong, Y.-S., Science of Synthesis, (2009) 46, 623. 摘要:Kwiecień, H., Science of Synthesis Knowledge Updates, (2018) 3, 134. 摘要:Hutskalova, V.; Sparr, C., Science of Synthesis Knowledge Updates, (2022) 1, 42. 摘要:Rudzinski, D. M.; Leadbeater, N. E., Science of Synthesis Knowledge Updates, (2012) 1, 372.